Evaluation of calibration curve-based approaches to predict clinical inducers and noninducers of CYP3A4 with plated human hepatocytes

Drug Metabolism and Disposition

Volumn 42, Issue 9, 2014, Pages 1379-1391

  Zhang, J George ^a   Ho, Thuy ^a   Callendrello, Alanna L ^a   Clark, Robert J ^a   Santone, Elizabeth A ^a   Kinsman, Sarah ^a   Xiao, Deqing ^a   Fox, Lisa G ^a   Einolf, Heidi J ^b   Stresser, David M ^a  

^a Corning Gentest Contract Research Services Corning Life Sciences ^*  (United States)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYP3A4 PROTEIN, HUMAN; CYTOCHROME P450 3A; DRUG; MESSENGER RNA; MIXED FUNCTION OXIDASE; TESTOSTERONE;

AREA UNDER THE CURVE; CALIBRATION; CELL CULTURE; CRYOPRESERVATION; ENZYME INDUCTION; FOOD AND DRUG ADMINISTRATION; GENETICS; HUMAN; LIVER CELL; METABOLISM; PROCEDURES; UNITED STATES;

AREA UNDER CURVE; CALIBRATION; CELLS, CULTURED; CRYOPRESERVATION; CYTOCHROME P-450 CYP3A; ENZYME INDUCTION; HEPATOCYTES; HUMANS; MIXED FUNCTION OXYGENASES; PHARMACEUTICAL PREPARATIONS; RNA, MESSENGER; TESTOSTERONE; UNITED STATES; UNITED STATES FOOD AND DRUG ADMINISTRATION;

EID: 84906874534     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.114.058602     Document Type: Article

References (43)

1. Adams M, Pieniaszek HJ, Jr, and Gammaitoni AR, andAhdieh H (2005) Oxymorphone extended release does not affect CYP2C9 or CYP3A4 metabolic pathways. J Clin Pharmacol 45:337-345. (Pubitemid 40490430)
2. Ahonen J, Olkkola KT, and Neuvonen PJ (1995) Effect of itraconazole and terbinafine on the pharmacokinetics and pharmacodynamics of midazolam in healthy volunteers. Br J Clin Pharmacol 40:270-272.
3. Almond LM, Yang J, Jamei M, Tucker GT, and Rostami-Hodjegan A (2009) Towards a quantitative framework for the prediction of DDIs arising from cytochrome P450 induction. Curr Drug Metab 10:420-432.
4. Backman JT, Olkkola KT, and Neuvonen PJ (1996a) Rifampin drastically reduces plasma concentrations and effects of oral midazolam. Clin Pharmacol Ther 59:7-13. (Pubitemid 26046768)
5. Backman JT, Olkkola KT, Ojala M, Laaksovirta H, and Neuvonen PJ (1996b) Concentrations and effects of oral midazolam are greatly reduced in patients treated with carbamazepine or phenytoin. Epilepsia 37:253-257. (Pubitemid 26071826)
6. Backman JT, Kivistö KT, Olkkola KT, and Neuvonen PJ (1998) The area under the plasma concentration-time curve for oral midazolam is 400-fold larger during treatment with itraconazole than with rifampicin. Eur J Clin Pharmacol 54:53-58. (Pubitemid 28189400)
7. Daly AK (2006) Significance of the minor cytochrome P450 3A isoforms. Clin Pharmacokinet 45:13-31.
8. Eap CB, Buclin T, Cucchia G, Zullino D, Hustert E, Bleiber G, Golay KP, Aubert AC, Baumann P, and Telenti A, et al. (2004) Oral administration of a low dose of midazolam (75 microg) as an in vivo probe for CYP3A activity. Eur J Clin Pharmacol 60:237-246. (Pubitemid 38916442)
9. Einolf HJ, Chen L, Fahmi OA, Gibson CR, Obach RS, Shebley M, Silva J, Sinz MW, Unadkat JD, and Zhang L, et al. (2014) Evaluation of various static and dynamic modeling methods to predict clinical CYP3A induction using in vitro CYP3A4 mRNA induction data. Clin Pharmacol Ther 95:179-188.
10. EMA (2013) Guideline on the investigation of drug interactions (final). http://www.ema.europa.eu/docs/en-GB/document-library/Scientific-guideline/2012/ 07/WC500129606.pdf.
11. Fahmi OA, Hurst S, Plowchalk D, Cook J, Guo F, Youdim K, Dickins M, Phipps A, Darekar A, and Hyland R, et al. (2009) Comparison of different algorithms for predicting clinical drug-drug interactions, based on the use of CYP3A4 in vitro data: predictions of compounds as precipitants of interaction. Drug Metab Dispos 37:1658-1666.
12. Fahmi OA, Kish M, Boldt S, and Obach RS (2010) Cytochrome P450 3A4 mRNA is a more reliable marker than CYP3A4 activity for detecting pregnane X receptor-activated induction of drug-metabolizing enzymes. Drug Metab Dispos 38:1605-1611.
13. Fahmi OA and Ripp SL (2010) Evaluation of models for predicting drug-drug interactions due to induction. Expert Opin Drug Metab Toxicol 6:1399-1416.
14. Fahmi OA, Raucy JL, Ponce E, Hassanali S, and Lasker JM (2012) Utility of DPX2 cells for predicting CYP3A induction-mediated drug-drug interactions and associated structure-activity relationships. Drug Metab Dispos 40:2204-2211.
15. FDA (2012) Guidance for industry - Drug interaction studies - study design, data analysis, implications for dosing, and labeling recommendations (draft guidance). http://www.fda.gov/downloads/Drugs/ GuidanceComplianceRegulatoryInformation/Guidances/ucm292362.pdf.
16. Furukori H, Otani K, Yasui N, Kondo T, Kaneko S, Shimoyama R, Ohkubo T, Nagasaki T, and Sugawara K (1998) Effect of carbamazepine on the single oral dose pharmacokinetics of alprazolam. Neuropsychopharmacology 18:364-369. (Pubitemid 28140661)
17. Gibbs MA, Kunze KL, Howald WN, and Thummel KE (1999) Effect of inhibitor depletion on inhibitory potency: tight binding inhibition of CYP3A by clotrimazole. Drug Metab Dispos 27:596-599. (Pubitemid 29214471)
18. Harris RZ, Inglis AM, Miller AK, Thompson KA, Finnerty D, Patterson S, Jorkasky DK, and Freed MI (1999) Rosiglitazone has no clinically significant effect on nifedipine pharmacokinetics. J Clin Pharmacol 39:1189-1194. (Pubitemid 30644023)
19. Inglis AM, Miller AK, Culkin KT, Finnerty D, Patterson SD, Jorkasky DK, and Freed MI (2001) Lack of effect of rosiglitazone on the pharmacokinetics of oral contraceptives in healthy female volunteers. J Clin Pharmacol 41:683-690. (Pubitemid 32493364)
20. Isoherranen N, Lutz JD, Chung SP, Hachad H, Levy RH, and Ragueneau-Majlessi I (2012) Importance of multi-p450 inhibition in drug-drug interactions: evaluation of incidence, inhibition magnitude, and prediction from in vitro data. Chem Res Toxicol 25:2285-2300.
21. Kanebratt KP andAndersson TB (2008) HepaRG cells as an in vitro model for evaluation of cytochrome P450 induction in humans. Drug Metab Dispos 36:137-145.
22. Kato M, Chiba K, Horikawa M, and Sugiyama Y (2005) The quantitative prediction of in vivo enzyme-induction caused by drug exposure from in vitro information on human hepatocytes. Drug Metab Pharmacokinet 20:236-243.
23. Kim KA, Oh SO, Park PW, and Park JY (2005) Effect of probenecid on the pharmacokinetics of carbamazepine in healthy subjects. Eur J Clin Pharmacol 61:275-280.
24. Kirby BJ, Collier AC, Kharasch ED, Whittington D, Thummel KE, and Unadkat JD (2011) Complex drug interactions of HIV protease inhibitors 1: inactivation, induction, and inhibition of cytochrome P450 3A by ritonavir or nelfinavir. Drug Metab Dispos 39:1070-1078.
25. Leizorovicz A, Piolat C, Boissel JP, Sanchini B, and Ferry S (1984) Comparison of two long-acting forms of quinidine. Br J Clin Pharmacol 17:729-734. (Pubitemid 14068507)
26. Livak KJ and Schmittgen TD (2001) Analysis of relative gene expression data using real-time quantitative PCR and the 2(-Δ Δ C(T)) Method. Methods 25:402-408. (Pubitemid 34164012)
27. Ma JD, Nafziger AN, Rhodes G, Liu S, and Bertino JS, Jr (2006) Duration of pleconaril effect on cytochrome P450 3A activity in healthy adults using the oral biomarker midazolam. Drug Metab Dispos 34:783-785.
28. McGinnity DF, Zhang G, Kenny JR, Hamilton GA, Otmani S, Stams KR, Haney S, Brassil P, Stresser DM, and Riley RJ (2009) Evaluation of multiple in vitro systems for assessment of CYP3A4 induction in drug discovery: human hepatocytes, pregnane X receptor reporter gene, and Fa2N-4 and HepaRG cells. Drug Metab Dispos 37:1259-1268.
29. Mihaly GW, Ching MS, Klejn MB, Paull J, and Smallwood RA (1987) Differences in the binding of quinine and quinidine to plasma proteins. Br J Clin Pharmacol 24:769-774. (Pubitemid 18078380)
30. Ohtsuki S, Schaefer O, Kawakami H, Inoue T, Liehner S, Saito A, Ishiguro N, Kishimoto W, Ludwig-Schwellinger E, and Ebner T, et al. (2012) Simultaneous absolute protein quantification of transporters, cytochromes P450, and UDP-glucuronosyltransferases as a novel approach for the characterization of individual human liver: comparison with mRNA levels and activities. Drug Metab Dispos 40:83-92.
31. O'Reilly RA (1982) Stereoselective interaction of sulfinpyrazone with racemic warfarin and its separated enantiomorphs in man. Circulation 65:202-207.
32. Prueksaritanont T, Vega JM, Zhao J, Gagliano K, Kuznetsova O, Musser B, Amin RD, Liu L, Roadcap BA, and Dilzer S, et al. (2001) Interactions between simvastatin and troglitazone or pioglitazone in healthy subjects. J Clin Pharmacol 41:573-581. (Pubitemid 32381875)
33. Ripp SL, Mills JB, Fahmi OA, Trevena KA, Liras JL, Maurer TS, and de Morais SM (2006) Use of immortalized human hepatocytes to predict the magnitude of clinical drug-drug interactions caused by CYP3A4 induction. Drug Metab Dispos 34:1742-1748. (Pubitemid 44427477)
34. Schellens JH, van der Wart JH, Brugman M, and Breimer DD (1989) Influence of enzyme induction and inhibition on the oxidation of nifedipine, sparteine, mephenytoin and antipyrine in humans as assessed by a "cocktail" study design. J Pharmacol Exp Ther 249:638-645. (Pubitemid 19144859)
35. Selen A, Amidon GL, and Welling PG (1982) Pharmacokinetics of probenecid following oral doses to human volunteers. J Pharm Sci 71:1238-1242. (Pubitemid 13230064)
36. Shimada T, Yamazaki H, Mimura M, Inui Y, and Guengerich FP (1994) Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians. J Pharmacol Exp Ther 270:414-423. (Pubitemid 24229655)
37. Shord SS, Chan LN, Camp JR, Vasquez EM, Jeong HY, Molokie RE, Baum CL, and Xie H (2010) Effects of oral clotrimazole troches on the pharmacokinetics of oral and intravenous midazolam. Br J Clin Pharmacol 69:160-166.
38. Shou M, Hayashi M, Pan Y, Xu Y, Morrissey K, Xu L, and Skiles GL (2008) Modeling, prediction, and in vitro in vivo correlation of CYP3A4 induction. Drug Metab Dispos 36:2355-2370.
39. Soons PA, van den Berg G, Danhof M, van Brummelen P, Jansen JB, Lamers CB, and Breimer DD (1992) Influence of single- and multiple-dose omeprazole treatment on nifedipine pharmacokinetics and effects in healthy subjects. Eur J Clin Pharmacol 42:319-324.
40. Wienkers LC and Heath TG (2005) Predicting in vivo drug interactions from in vitro drug discovery data. Nat Rev Drug Discov 4:825-833. (Pubitemid 41553963)
41. Williams JA, Ring BJ, Cantrell VE, Jones DR, Eckstein J, Ruterbories K, Hamman MA, and Hall SD, andWrighton SA (2002) Comparative metabolic capabilities of CYP3A4, CYP3A5, and CYP3A7. Drug Metab Dispos 30:883-891. (Pubitemid 34815417)
42. Xu Y, Zhou Y, Hayashi M, Shou M, and Skiles GL (2011) Simulation of clinical drug-drug interactions from hepatocyte CYP3A4 induction data and its potential utility in trial designs. Drug Metab Dispos 39:1139-1148.
43. Zhang JG, Ho T, Callendrello AL, Crespi CL, and Stresser DM (2010) A multi-endpoint evaluation of cytochrome P450 1A2, 2B6 and 3A4 induction response in human hepatocyte cultures after treatment with β-naphthoflavone, phenobarbital and rifampicin. Drug Metab Lett 4:185-194.